In vitro antioxidant and pancreatic anticancer activity of novel 5-fluorouracil-coumarin conjugates
Molecular hybridization consists of the combination of two or more non-identical pharmaco-phores in a single molecule. It has emerged as a promising strategy that allows the design of mo-lecular frameworks with enhanced activity and affinity compared to their parent drugs. In this work, two novel hy...
| Autores: | , , , , , , |
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| Tipo de documento: | artigo |
| Data de publicação: | 2022 |
| País: | España |
| Recursos: | Universidad de Castilla-La Mancha |
| Repositório: | RUIdeRA. Repositorio Institucional de la UCLM |
| OAI Identifier: | oai:ruidera.uclm.es:10578/32460 |
| Acesso em linha: | https://doi.org/10.3390/pharmaceutics14102152 https://hdl.handle.net/10578/32460 |
| Access Level: | Acceso aberto |
| Palavra-chave: | 5-Fluorouracil Anticancer Antioxidant Click chemistry Conjugates Coumarins. |
| Resumo: | Molecular hybridization consists of the combination of two or more non-identical pharmaco-phores in a single molecule. It has emerged as a promising strategy that allows the design of mo-lecular frameworks with enhanced activity and affinity compared to their parent drugs. In this work, two novel hybrids that combine the well-known anticancer chemotherapeutic agent 5-fluorouracil with antioxidant coumarin derivatives have been synthesized and characterized by means of a copper-catalyzed azide-alkyne cycloaddition (CuAAC). The conjugates showed good antioxidant properties and a high tendency to aggregate and form stable nanoparticles in aque-ous media, with regular shape and uniform size. These materials have proven to be preferential cytotoxic agents in vitro against human pancreatic cancer cells PANC-1, with an activity superior to free 5-fluorouracil. These results open up the possibility of exploiting the synergistic combina-tion between 5-fluorouracil and coumarin derivatives and warrant further investigation of these hybrids as promising pancreatic anticancer agents. |
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